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    Curr Opin Drug Discov Devel. 2010 Sep;13(5):577-86.

    Small-molecule PARP modulators--current status and future therapeutic potential.

    Penning TD.

    Source

    Abbott Laboratories, Cancer Research, Global Pharmaceutical Research and Development, 100 Abbott Park Road, Abbott Park, IL 60064, USA. thomas.penning@abbott.com

    Abstract

    PARP-1 inhibitors have emerged as a promising therapeutic class of compounds, and numerous PARP inhibitors, including iniparib (BiPar Sciences Inc/sanofi-aventis), olaparib (AstraZeneca plc), veliparib (Abbott Laboratories), PF-1367338 (Pfizer Inc), MK-4827 (Merck & Co Inc) and CEP-9722 (Cephalon Inc), have advanced into clinical trials. Several additional inhibitors are expected to enter clinical trials within the next year. Early investigations with PARP-1 inhibitors involved non-oncological indications, but development has since progressed to focus primarily on oncology, for use both as single chemotherapeutic agents in specific patient populations (eg, BRCA-deficient) and as combination therapies with various chemotherapeutics. This review focuses on new developments in lead clinical PARP inhibitors, recent disclosures of new inhibitors and the potential use of PARP-1 inhibitors in new disease settings.

    PMID:
    20812149
    [PubMed - indexed for MEDLINE]

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